An improved synthesis of pyrido[2,3-<i>d</i>]pyrimidin-4(1<i>H</i>)-ones and their antimicrobial activity

Farès, Mohamed; Hadi, Soha R. Abd El; Eladwy, Radwa A.; Shoun, Aly A.; Abdel‐Aziz, Marwa M.; Eldehna, Wagdy M.; Abdel‐Aziz, Hatem A.; Keller, P. A.

doi:10.1039/c8ob00627j

Cited by 22 publications

(18 citation statements)

References 28 publications

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“…Synthesis of 7-Amino-3-phenyl [1,2,4]triazolo [4,3-a]pyrimidin-5(1H)-one (57). Fares et al 87 reported that some of the synthesized pyrido [2,3-d]pyrimidine derivatives displayed antimicrobial and anti-fungal activities. Among the tested derivatives, compound 63 (R 1 = 4-Cl-C6H4, R 2 = C6H5) was found to exhibit the most potent effect against Streptococcus pneumoniae and Escherichia coli.…”

Section: Table 8 Synthesis Of Compounds 54a-lmentioning

confidence: 99%

Aminouracil and aminothiouracil as versatile precursors for a variety of heterocyclic systems

Diab¹,

Salem²,

Abdelhamid³

et al. 2021

Arkivoc

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Heterocycles, particularly pyrimidine derivatives, which are present in many natural products and many interesting synthetic compounds, are the most diverse class of organic compounds and have significant chemical, biomedical and industrial applications. Uracil, a pyrimidine derivative, constitutes a promising structure in widespread natural products and many of its derivatives exhibited significant pharmacological properties. They have been widely used as starting materials for the synthesis of a huge number of biologically important nitrogen-containing heterocycles. This review casts light on various methods for the construction of different heterocyclic systems utilizing aminouracil and aminothiouracil as versatile precursors. The heterocyclic systems mentioned in this review are categorized according to the type of the heterocyclic systems.

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Section: Table 8 Synthesis Of Compounds 54a-lmentioning

confidence: 99%

Aminouracil and aminothiouracil as versatile precursors for a variety of heterocyclic systems

Diab¹,

Salem²,

Abdelhamid³

et al. 2021

Arkivoc

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show abstract

“…The antimicrobial action of compound 30a had shown MIC = 0.49-7.81 μg/ml and discrimination index was more than the normal against CCD-33Co cell line. Further, the antifungal action of derivatives 31a, 31b and 31c were found moderate to strong (Fares et al, 2018). Naeimi and co-workers synthesized an effective and appropriate pyrido [2,3-d: 6,5-d′] dipyrimidine derivatives through simple one pot, multicomponent reaction protocol of 2-thiobarbiturate, ammonium acetate and substituted aromatic aldehyde by condensation in the presence of [H-NMP] + [HSO 4 ] − as a catalyst.…”

Section: Anti-infectious Agentsmentioning

confidence: 99%

An overview on synthetic and pharmaceutical prospective of pyrido[2,3‐d]pyrimidines scaffold

Yadav

Shah

2020

Chem Biol Drug Des

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Pyrido[2,3-d]pyrimidine, a fused hetero-bicyclic nucleus containing pyridine and pyrimidine rings has attained the momentary attention in the sphere of multicomponent synthetic protocol and medicinal chemist. Pyrido[2,3-d]pyrimidine derived drugs have manifested diverse pharmacological activities, particularly, anti-inflammatory, cytotoxic, antimicrobial, phosphodiesterase inhibitors and cytokine inhibitors etc. The present review illustrates various modern synthetic strategies adopted, the structure-activity relationship (SAR) aspects and discloses the extensive crucial biological properties (anticancer, anti-infectious, anti-diabetics and CNS agents) of pyrido[2,3-d]pyrimidines. K E Y W O R D S anticancer, anti-diabetics, anti-infectious, CNS agents, pyrido[2,3-d]pyrimidines How to cite this article: Yadav P, Shah K. An overview on synthetic and pharmaceutical prospective of pyrido[2,3-d]pyrimidines scaffold.

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“…In the current situation, several heterocycles have emerged presenting a vital role in many medicinal agents, which have a direct impact on the health of mankind. Among these, pyrimidine turned to play a vital role in a broad range of pharmacological potential like anticancer, [ 2 ] antimicrobial, [ 3–5 ] antiinflammatory, antiviral, [ 6 ] anxiolytic, and anticonvulsant. It is an aromatic heterocycle comprising two nitrogen atoms at the first and third positions and four carbon atoms.…”

Section: Introductionmentioning

confidence: 99%

Microwave‐assisted diversified synthesis of pyrimidines: An overview

Kumar

2021

Journal of Heterocyclic Chem

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Pyrimidines and their hybrid molecules have continued to be a favorable area for organic chemists owing to their richness in natural and synthetic compounds with multifarious involvement in pharmaceuticals and polymers and act as ligands. Different novel and greener synthetic protocols were developed in the last decades, but microwave‐assisted synthetic protocols played a significant role in constructing pyrimidine and its derivatives. In this article, we summarized the microwave‐supported strategy for the construction of pyrimidine fused or linked/tethered with other heterocycles, polysubstituted pyrimidines, solid‐supported synthesis of pyrimidines, and ionic liquid‐catalyzed strategies for the synthesis of pyrimidine and its derivatives reported in the last decade. Solid‐supported protocols using resins and ionic liquid‐catalyzed strategies afforded the corresponding products with excellent yield by dual activation. In most of the reports, the microwave‐irradiated approach was compared with conventional/traditional heating and found better in terms of reaction time, yield, atom economy, adherence with green chemistry principles, and reduction in purification wastage. Various authors evaluated the in vitro potential of synthesized pyrimidine derivatives for antimicrobial and antimalarial potential, and found moderate to excellent biological activity.

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An improved synthesis of pyrido[2,3-d]pyrimidin-4(1H)-ones and their antimicrobial activity

Cited by 22 publications

References 28 publications

Aminouracil and aminothiouracil as versatile precursors for a variety of heterocyclic systems

Aminouracil and aminothiouracil as versatile precursors for a variety of heterocyclic systems

An overview on synthetic and pharmaceutical prospective of pyrido[2,3‐d]pyrimidines scaffold

Microwave‐assisted diversified synthesis of pyrimidines: An overview

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